Formula of liposome preparation containing compound amino acid and preparation method thereof

A liposome preparation and compound amino acid technology, applied in liposome delivery, medical preparations containing active ingredients, pharmaceutical formulas, etc., to achieve the effect of promoting wound healing, keeping moist, and blocking secondary infection

Active Publication Date: 2012-07-04
GUIZHOU YANGSHENG MEDICAL INSTR
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Yet up to now, also do not adopt any organic solvent, liposome encapsulation rate is high, the stability of preparation is good, the preparation technology of the liposome preparation that can realize industrialized large-scale production comes out

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment l

[0021] First weigh 25g of soybean lecithin and 7g of cholesterol, put them in a clean container, heat 161ml of processing water to 60°C, stir for 100min, and control the speed of the stirring blade at 3500r / min to obtain the oil phase;

[0022] Then take by weighing cysteine ​​hydrochloride 0.3g, tryptophan 0.15g put in clean container, process water 646ml after dissolving, then add valine 1.25g, isoleucine 0.83g, leucine 1.62g, Lysine acetate 0.79g, methionine 0.48g, phenylalanine 0.53g, threonine 0.15g, arginine 0.15g, glycine 0.21g, proline 0.09g; then add auxiliary materials vitamin A0.3g, vitamin C 0.82g, vitamin E 0.50g, vitamin K 0.03g, sodium alginate (sodium alginate) 151.9g, finally add 0.9g potassium sorbate, stir to dissolve and mix, and obtain the water phase;

[0023] Afterwards, the oil phase and the water phase are mixed, and sheared by a high-speed shearing machine to make a liposome preparation with a particle size of less than 200 nm.

Embodiment 2

[0025] First weigh 140g of soybean lecithin and 80g of cholesterol, put them in a clean container, heat 350ml of processing water to 72°C, stir for 120min, and control the speed of the stirring blade at 5100r / min to obtain the oil phase;

[0026] Then take by weighing cysteine ​​hydrochloride 0.30g, tryptophan 0.31g put in clean container, after processing process water 340ml dissolve, then add valine 0.41g, isoleucine 0.84g, leucine 1.93g, Lysine acetate 0.99g, methionine 0.15g, phenylalanine 0.16g, threonine 0.36g, arginine 0.47g, glycine 0.58g, proline 0.09g; then add auxiliary materials vitamin A 0.21g, vitamin C 0.45g, vitamin E 0.31g, vitamin K 0.04g, sodium alginate (sodium alginate) 81.9g, finally add 0.5g potassium sorbate, stir to dissolve and mix, and obtain the water phase;

[0027] Afterwards, the oil phase and the water phase are mixed, and sheared by a high-speed shearing machine to make a liposome preparation with a particle size of less than 200 nm.

Embodiment 3

[0029] First weigh 25g of soybean lecithin and 9g of cholesterol into a clean container, heat 250ml of processing water to 70°C, stir for 60min, and control the speed of the stirring blade at 3500r / min to obtain the oil phase;

[0030] Then weigh 0.61g of cysteine ​​hydrochloride and 0.39g of tryptophan, put them in a clean container, dissolve them in 573 ml of processing water, then add 1.01g of valine, 0.66g of isoleucine, and 1.95g of leucine in sequence , 0.36g of lysine acetate, 0.27g of methionine, 0.38g of phenylalanine, and 0.44g of threonine; then add 0.41g of vitamin C, 135.2g of sodium alginate (sodium brown acid) in sequence, and finally add sorbic acid Potassium 1.32g, stir to make it dissolve and mix, and obtain the water phase;

[0031] Afterwards, the oil phase and the water phase are mixed, and sheared by a high-speed shearing machine to make a liposome preparation with a particle size of less than 200 nm.

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Abstract

The invention discloses a formula of a liposome preparation containing compound amino acids and a preparation method thereof; a raw material mass ratio of the liposome preparation is determined; the preparation method comprises the following steps: (1) weighing soybean phosphatide and cholesterol, adding water, heating and stirring to prepare an oil phase; (2) weighing cysteine hydrochloride and tryptophan, adding process water for dissolution, orderly adding some or all of valine, isoleucine, leucine, lysine acetate, methionine, phenylalanine, threonine, arginine, glycine, and praline; then orderly adding one or more than one of auxiliary materials of vitamin A, vitamin C, vitamin E, and vitamin K, and a film forming material, finally adding potassium sorbate or ethylparaben, stirring toprepare a water phase; (3) mixing the oil phase and the water phase, shearing by a high-speed shearing machine to obtain the liposome preparation. The invention initiates the technology for preparingliposome without the adoption of any organic solvents; the prepared liposome preparation has high entrapment efficiency, and good stability; and industrial production is realized.

Description

technical field [0001] The invention relates to a pharmaceutical preparation characterized by a special physical shape, in particular to a liposome preparation containing compound amino acid components. Background technique [0002] The development of liposome technology has a history of nearly 50 years. The current liposome preparation methods mainly fall into four categories: 1) Detergent dialysis, but this method is difficult to industrialize and is not suitable for encapsulating water-soluble drugs ; 2) Based on the film dispersion method, the phospholipids used to form liposomes are dissolved in organic solvents—usually chloroform, a mixture of chloroform and methanol, anhydrous ether, tert-butanol, etc. The solvent was removed under pressure to form a dry phospholipid film. The phospholipid membranes are hydrated to form multilamellar vesicles. Although this method is the most classic method, there are many disadvantages, such as: the use of highly toxic organic solv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/405A61K31/401A61K31/198A61K31/195A61K9/127A61P3/02A61P17/02
Inventor 黄昌平郑茂鑫聂开品
Owner GUIZHOU YANGSHENG MEDICAL INSTR
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